Endocrinology- Pharmacology Flashcards
Diabetes mellitus management
Type 1 DM
Type 2 DM
Gestational DM
Insulin replacement
Oral agents (metformin is first line), non-insulin injectables, insulin replacement;
Insulin replacement if nutrition therapy and exercise alone fail.
*Regular (short-acting) insulin is preferred for DKA (IV), hyperkalemia (+ glucose), stress hyperglycemia.
Insulin preparations (injectables)
- Rapid acting
- Short acting
- Intermediate acting
- Long acting
(1hr peak): Lispro, Aspart, Glulisine (LAG)
(2 hrs peak) regular
(4-10 hrs peak) NPH
(not real peak) detemir, glargine, degludec
Diabtes drugs (injectables)
- Amylin analogs
- GLP-1 analogs
Pramlintide (Hypoglycemia, nausea)
Exenatide, liraglutide (Nausea, vomiting, pancreatitis.
Promote weight loss)
Biguanides
- Metformin
Inhibit hepatic gluconeogenesis and the action of glucagon, by inhibiting mGPD.
GI upset, lactic acidosis (use with caution in renal insufficiency), B12 deficiency. Promote weight loss.
Sulfonylureas
- 1st generation: chlorpropamide, tolbutamide
- 2nd generation: glimepiride, glipizide, glyburide
Close K+ channel in pancreatic β cell membrane.
Hypoglycemia (risk with renal failure), weight gain.
1st generation: disulfiram-like effects.
2nd generation: hypoglycemia.
Meglitinides
- Nateglinide, repaglinide
Close K+ channel in pancreatic β cell membrane.
Hypoglycemia (risk with renal failure), weight gain.
DPP-4 inhibitors
- Linagliptin, saxagliptin, sitagliptin
Inhibit DPP-4 enzyme that deactivates GLP-1.
Mild urinary or respiratory infections, weight neutral.
Glitazones/thiazolidinediones
- Pioglitazone, rosiglitazone
Binds to PPAR-γ nuclear transcription regulator.
Weight gain, edema, HF, risk of fractures.
Delayed onset of action (several weeks).
Sodium-glucose cotransporter 2 (SGLT2) inhibitors
- Canagliflozin, dapagliflozin, empagliflozin
Block reabsorption of glucose in proximal convoluted tubule.
Glucosuria, UTIs, vaginal yeast infections, hyperkalemia, dehydration (orthostatic hypotension), weight loss.
α-glucosidase inhibitors
- Acarbose, miglitol
Inhibit intestinal brush-border α-glucosidases
GI upset. Not recommended if kidney function is impaired.
Thioamides
- Names
- Mechanism
- Adverse effects
Propylthiouracil (PTU), methimazole.
Block thyroid peroxidase, PTU also blocks 5′-deiodinase.
Skin rash, agranulocytosis (rare), aplastic anemia, hepatotoxicity. Methimazole is a possible teratogen (can cause aplasia cutis).
Thioamides
- Clinical use
Hyperthyroidism. PTU used in first trimester of pregnancy. methimazole used in second and third trimesters of pregnancy.
- Not used to treat Graves ophthalmopathy (treated
with corticosteroids)
Levothyroxine (T4), liothyronine (T3)
- Mechanism
- Clinical use
- Adverse effects
Thyroid hormone replacement.
Hypothyroidism, myxedema. May be abused for weight loss.
Tachycardia, heat intolerance, tremors, arrhythmias.
Hypothalamic/pituitary drugs
- ADH antagonists (conivaptan, tolvaptan)
- Desmopressin
- GH
SIADH, block action of ADH at V2-receptor.
Central (not nephrogenic) DI, von Willebrand disease, sleep enuresis, hemophilia A.
GH deficiency, Turner syndrome
Hypothalamic/pituitary drugs
- Oxytocin
- Somatostatin (octreotide)
Labor induction (stimulates uterine contractions), milk letdown; controls uterine hemorrhage
Acromegaly, carcinoid syndrome, gastrinoma, glucagonoma, esophageal varices.
